Firategrast_product_DataBase

Bioactivity

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity[1][2][3].

Invitro

Firategrast (0.1-10 µM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cells adhesion[2]. Firategrast is a potent Integrin α4β1 (VLA-4) antagonist (IC50=198 nM) at inhibiting the binding of soluble VCAM/Fc chimeric protein (sVCAM-1) to G2 acute lymphoblastic leukemia (ALL) cells. VLA-4 is composed of CD49d (α4) and CD29 (β1)[1][4].

In Vivo

Firategrast (30 mg/kg/day in drinking water; starting 2 or 7 days post transplantation to 21 days) shows an overall reduction of leukemic cells in the spleen[3]. Animal Model:

Name

Firategrast

CAS

402567-16-2

Formula

C27H27F2NO6

Molar Mass

499.50

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Moses O. Evbuomwan, et al. Generation and Characterization of Novel VLA-4 Inhibitors for Stem Cell Mobilization in Combination with a CXCR2 Agonist. Blood (2017) 130 (Supplement 1): 3197. [2]. Sarah E M Herman, et al. Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In Vivo. Clin Cancer Res. 2015 Oct 15;21(20):4642-51. [3]. Eva Szenes, et al. TCL1 transgenic mice as a model for CD49d-high chronic lymphocytic leukemia. Leukemia. 2020 Sep;34(9):2498-2502. [4]. H Rahimi, et al. Aberrant regulation of the integrin very late antigen-4 in systemic lupus erythematosus. Lupus. 2013 Mar;22(3):297-306.

PeptideDB

Firategrast

CAS: 402567-16-2 F: C27H27F2NO6 W: 499.50